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(Reference retrieved automatically from Web of Science through information on FAPESP grant and its corresponding number as mentioned in the publication by the authors.)

Single-Pass Intestinal Perfusion (SPIP) and prediction of fraction absorbed and permeability in humans: A study with antiretroviral drugs

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Author(s):
Dezani, Thaisa Marinho [1] ; Dezani, Andre Bersani [1] ; da Silva Junior, Joao Batista [1] ; dos Reis Serra, Cristina Helena [1]
Total Authors: 4
Affiliation:
[1] Univ Sao Paulo, Fac Pharmaceut Sci, Dept Pharm, Ave Prof Lineu Prestes 580, Bl-13, BR-05508900 Sao Paulo, SP - Brazil
Total Affiliations: 1
Document type: Journal article
Source: EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS; v. 104, p. 131-139, JUL 2016.
Web of Science Citations: 14
Abstract

In recent years, the prediction of oral drug absorption in humans has been a challenge for researchers and many techniques for permeability studies have been developed for several purposes, including biowaiver processes. The Single-Pass Intestinal Perfusion (SPIP) method performed in rats can provide permeability results closest to in vivo condition. The purpose of the present study was to evaluate the intestinal permeability of the antiretroviral drugs lamivudine, stavudine and zidovudine using the SPIP method in rats and to predict their permeability (P-eff,P-humans) and fraction absorbed (F-a) in humans. Metoprolol and fluorescein were used as marker compounds of high and low permeability, respectively. The effective permeability (P-eff) results showed that stavudine and zidovudine have high permeability characteristics while lamivudine presented the lowest result. From P-eff values obtained in rats, the P-eff,P-humans and F-a were calculated. The use of SPIP in rats and calculations for absorption prediction in humans may indicate the transport mechanisms and/or pre-systemic metabolism involved on permeation processes of drugs, since this model is the closest to in vivo conditions. (C) 2016 Elsevier B.V. All rights reserved. (AU)

FAPESP's process: 11/09670-3 - Permeability study of antiretroviral drugs by in situ perfusion model. Application in the Biopharmaceutical Classification.
Grantee:João Batista da Silva Junior
Support Opportunities: Scholarships in Brazil - Scientific Initiation